Bioorg Med Chem Lett. 2008 Jul 15;18(14):4215-8. doi: 10.1016/j.bmcl.2008.05.059. Epub 2008 May 20.

Synthesis and screening of small molecule inhibitors of anthrax edema factor.

Jimenez ME, Bush K, Pawlik J, Sower L, Peterson JW, Gilbertson SR.

Source

Chemical Biology Program, Department of Pharmacology and Toxicology, The University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555-0650, USA.

Abstract

The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts of the prostaglandin PGE(2) reduce the net secretory response of cholera toxin-challenged mice and act directly on the action of anthrax edema factor, a calmodulin-dependent adenylyl cyclase. The simple enones examined in this letter were prepared by palladium-catalyzed Suzuki reaction.

PMID:: 18539457; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Supplemental Content

Save items

Related citations in PubMed

Discovery of a small molecule that inhibits the interaction of anthrax edema factor with its cellular activator, calmodulin. [Chem Biol. 2004]
Discovery of a small molecule that inhibits the interaction of anthrax edema factor with its cellular activator, calmodulin.
Lee YS, Bergson P, He WS, Mrksich M, Tang WJ. Chem Biol. 2004 Aug; 11(8):1139-46.
Structure-based inhibitor discovery against adenylyl cyclase toxins from pathogenic bacteria that cause anthrax and whooping cough. [J Biol Chem. 2003]
Structure-based inhibitor discovery against adenylyl cyclase toxins from pathogenic bacteria that cause anthrax and whooping cough.
Soelaiman S, Wei BQ, Bergson P, Lee YS, Shen Y, Mrksich M, Shoichet BK, Tang WJ. J Biol Chem. 2003 Jul 11; 278(28):25990-7. Epub 2003 Apr 3.
Review Quickening the pace of anthrax research: three advances point towards possible therapies. [Trends Microbiol. 2002]
Review Quickening the pace of anthrax research: three advances point towards possible therapies.
Chaudry GJ, Moayeri M, Liu S, Leppla SH. Trends Microbiol. 2002 Feb; 10(2):58-62.
Review The adenylyl cyclase activity of anthrax edema factor. [Mol Aspects Med. 2009]
Review The adenylyl cyclase activity of anthrax edema factor.
Tang WJ, Guo Q. Mol Aspects Med. 2009 Dec; 30(6):423-30. Epub 2009 Jun 26.
Crystallization and preliminary X-ray study of the edema factor exotoxin adenylyl cyclase domain from Bacillus anthracis in the presence of its activator, calmodulin. [Acta Crystallogr D Biol Crysta...]
Crystallization and preliminary X-ray study of the edema factor exotoxin adenylyl cyclase domain from Bacillus anthracis in the presence of its activator, calmodulin.
Drum CL, Shen Y, Rice PA, Bohm A, Tang WJ. Acta Crystallogr D Biol Crystallogr. 2001 Dec; 57(Pt 12):1881-4. Epub 2001 Nov 21.

See reviews... See all...

Cited by 2 PubMed Central articles

Design, synthesis, and diversification of 3,5-substituted enone library. [ACS Comb Sci. 2011]
Design, synthesis, and diversification of 3,5-substituted enone library.
Khalaf J, Estrella-Jimenez ME, Shashack MJ, Phatak SS, Zhang S, Gilbertson SR. ACS Comb Sci. 2011 Jul 11; 13(4):351-6. Epub 2011 Jun 22.
Testing the efficacy and toxicity of adenylyl cyclase inhibitors against enteric pathogens using in vitro and in vivo models of infection. [Infect Immun. 2010]
Testing the efficacy and toxicity of adenylyl cyclase inhibitors against enteric pathogens using in vitro and in vivo models of infection.
Moen ST, Blumentritt CA, Slater TM, Patel SD, Tutt CB, Estrella-Jimenez ME, Pawlik J, Sower L, Popov VL, Schein CH, et al. Infect Immun. 2010 Apr; 78(4):1740-9. Epub 2010 Feb 1.

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
BioAssay
PubChem BioAssay experiments on the biological activities of small molecules that cite the current articles. The depositors of BioAssay data provide these references.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Synthesis and screening of small molecule inhibitors of anthrax edema factor.
Synthesis and screening of small molecule inhibitors of anthrax edema factor.
Bioorg Med Chem Lett. 2008 Jul 15 ;18(14):4215-8. doi: 10.1016/j.bmcl.2008.05.059. Epub 2008 May 20 .

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Result Filters

Display Settings:

Send to:

Synthesis and screening of small molecule inhibitors of anthrax edema factor.

Source

Abstract

Publication Types, MeSH Terms, Substances

Publication Types

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Chemical Information

Medical

Molecular Biology Databases

Supplemental Content

Save items

Related citations in PubMed

Cited by 2 PubMed Central articles

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information